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Small-Molecule Activators of a Proenzyme

2009; American Association for the Advancement of Science; Volume: 326; Issue: 5954 Linguagem: Inglês

10.1126/science.1177585

1095-9203

Dennis W. Wolan, Julie A. Zorn, Daniel C. Gray, James A. Wells,

Mitochondrial Function and Pathology

Small-Molecule Protease Activator Human proteases regulate numerous biological processes. Most are stored as inactive proenzymes that are activated either by upstream processes or by self-proteolysis. Wolan et al. (p. 853 ) have identified a small molecule that activates the apoptotic procaspases-3 and -6. These caspases are homodimers, and the compound probably competitively inhibits one active site, but stabilizes an on-state conformation that promotes self-cleavage by the unoccupied site. It may thus be possible to find other small-molecule activators for other proenzymes that should facilitate functional and mechanistic studies.